WO2004087695A1 - Verfahren zur herstellung von pyrrolidin-1,2-dicarbonsäure-1-(phenyl(-amid))-2-(phenyl(-amid)) derivaten und 1-(phenylcarbamoyl)-pyrrolidin-2-carbonsäure derivate als zwischenprodukte - Google Patents
Verfahren zur herstellung von pyrrolidin-1,2-dicarbonsäure-1-(phenyl(-amid))-2-(phenyl(-amid)) derivaten und 1-(phenylcarbamoyl)-pyrrolidin-2-carbonsäure derivate als zwischenprodukte Download PDFInfo
- Publication number
- WO2004087695A1 WO2004087695A1 PCT/EP2004/002405 EP2004002405W WO2004087695A1 WO 2004087695 A1 WO2004087695 A1 WO 2004087695A1 EP 2004002405 W EP2004002405 W EP 2004002405W WO 2004087695 A1 WO2004087695 A1 WO 2004087695A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- amide
- oxo
- phenyl
- formula
- pyrrolidine
- Prior art date
Links
- 0 CC1(*)/C=C/C(/NC(C(C*(*)CC2)N2C(Nc2ccc(*)cc2)=O)=O)=C\*(*)/C=C1 Chemical compound CC1(*)/C=C/C(/NC(C(C*(*)CC2)N2C(Nc2ccc(*)cc2)=O)=O)=C\*(*)/C=C1 0.000 description 3
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Definitions
- Hai F, Cl, Br or I and their pharmaceutically usable derivatives, solvates and stereoisomers, including mixtures thereof in all ratios, characterized in that a) a compound of formula II
- the inhibition of factor VIIa and the measurement of the anticoagulant and antithrombotic activity can be determined by conventional in vitro or in vivo methods.
- a common method of measuring the inhibition of factor VIIa is described, for example, in US Pat. by H.F. Ronning et al. in Thrombosis Research 1996, 84, 73-81.
- R 3 is 2-oxopiperidin-1-yl, 2-oxopyrrolidin-1-yl, 2-oxo-1H-pyridin-1-yl, 3-oxomorpholin-4-yl , 4-oxo-1H-pyridin-1-yl, 2-oxo-1H-pyrazino-1-yl, 2-oxo-imidazolidin-1-yl, 2-oxo-piperazine-1-yl or 3-oxo -2H-pyridazin-2-yl.
- R 1 is H, OH or OA
- R 2 is H, shark or A
- A is unbranched, branched or cyclic alkyl having 1 -10 C
- Atoms in which also 1-7 H atoms may be replaced by F, Hal, F, Cl, Br or I, and their pharmaceutically usable derivatives, solvates and stereoisomers, including mixtures thereof in all ratios.
- EEDQ ethyl 2-ethoxy-1, 2-dihydroquinoline-1-carboxylate
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Description
Claims
Priority Applications (9)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04718646A EP1608646B1 (de) | 2003-04-03 | 2004-03-09 | Verfahren zur herstellung von pyrrolidin-1,2-dicarbonsäure-1 -(phenyl(-amid))-2-(phenyl(-amid)) derivaten und 1-(phenylcarbamoyl)-pyrrolidin-2-carbonsäurederivate als zwischenprodukte |
JP2006504602A JP4634369B2 (ja) | 2003-04-03 | 2004-03-09 | 1−n−(フェニル)−2−n−(フェニル)ピロリジン−1,2−ジカルボキサミド誘導体の製造方法および中間体としての1−(フェニルカルバモイル)ピロリジン−2−カルボン酸誘導体 |
MXPA05010433A MXPA05010433A (es) | 2003-04-03 | 2004-03-09 | Derivados de pirrolidina y procedimiento para prepararlos. |
US10/551,670 US7504500B2 (en) | 2003-04-03 | 2004-03-09 | Method for the production of pyrrolidine-1,2-dicarboxylic acid-1-(phenyl(-amide))-2(phenyl(-amide)) derivatives and 1-(phenylcarbamoyl)-pyrrolidine-2-carboxylic acid derivatives as intermediate products |
BRPI0408888-3A BRPI0408888A (pt) | 2003-04-03 | 2004-03-09 | processo para a preparação de derivados de 1-n-(fenil)-2-n-(fenil) pirrolidina-1,2-dicarboxamida e derivados de ácido 1-(fenilcarbamoil) pirrolidina-2-carboxìlico como intermediários |
DE502004004294T DE502004004294D1 (de) | 2003-04-03 | 2004-03-09 | Verfahren zur herstellung von pyrrolidin-1,2-dicarbonsäure-1 -(phenyl(-amid))-2-(phenyl(-amid)) derivaten und 1-(phenylcarbamoyl)-pyrrolidin-2-carbonsäurederivate als zwischenprodukte |
ES04718646T ES2287708T3 (es) | 2003-04-03 | 2004-03-09 | Metodo para la produccion de derivados de acido pirrolidin-1,2-dicarboxilico-ii-(fenil(-amida)-2-(fenil-amida)y derivados del acido 1-(fenilcarbamoil)-pirrolidina-2-carboxilico como productos intermediarios. |
CA2520893A CA2520893C (en) | 2003-04-03 | 2004-03-09 | Process for the preparation of 1-n-(phenyl)-2-n-(phenyl)pyrrolidine-1,2-dicarboxamide derivatives and 1-(phenylcarbamoyl)pyrrolidine-2-carboxylic acid derivatives as intermediates |
AU2004226280A AU2004226280B2 (en) | 2003-04-03 | 2004-03-09 | Method for the production of pyrrolidine-1,2-dicarboxylic acid-1-(phenyl(-amide))-2-(phenyl(-amide)) derivatives and 1-(phenylcarbamoyl)-pyrrolidine-2-carboxylic acid derivatives as intermediate products |
Applications Claiming Priority (10)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10315377A DE10315377A1 (de) | 2003-04-03 | 2003-04-03 | Carbonylverbindungen |
DE10315377.2 | 2003-04-03 | ||
DE10327428.6 | 2003-06-18 | ||
DE10327428A DE10327428A1 (de) | 2003-06-18 | 2003-06-18 | Ethinylprolinderivate |
DE2003129295 DE10329295A1 (de) | 2003-06-30 | 2003-06-30 | Carbonylverbindungen |
DE10329295.0 | 2003-06-30 | ||
DE10329457A DE10329457A1 (de) | 2003-04-03 | 2003-07-01 | Ethinylprolinderivate |
DE10329457.0 | 2003-07-01 | ||
DE2003134174 DE10334174A1 (de) | 2003-07-26 | 2003-07-26 | Pyrrolidinderivate und Verfahren zur Herstellung |
DE10334174.9 | 2003-07-26 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2004087695A1 true WO2004087695A1 (de) | 2004-10-14 |
Family
ID=33136213
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/EP2004/002405 WO2004087695A1 (de) | 2003-04-03 | 2004-03-09 | Verfahren zur herstellung von pyrrolidin-1,2-dicarbonsäure-1-(phenyl(-amid))-2-(phenyl(-amid)) derivaten und 1-(phenylcarbamoyl)-pyrrolidin-2-carbonsäure derivate als zwischenprodukte |
Country Status (16)
Country | Link |
---|---|
US (1) | US7504500B2 (de) |
EP (1) | EP1608646B1 (de) |
JP (1) | JP4634369B2 (de) |
KR (1) | KR20050118709A (de) |
AR (1) | AR043831A1 (de) |
AT (1) | ATE366732T1 (de) |
AU (1) | AU2004226280B2 (de) |
BR (1) | BRPI0408888A (de) |
CA (1) | CA2520893C (de) |
DE (2) | DE10329457A1 (de) |
ES (1) | ES2287708T3 (de) |
MX (1) | MXPA05010433A (de) |
PE (1) | PE20050395A1 (de) |
PL (1) | PL377138A1 (de) |
TW (1) | TW200500339A (de) |
WO (1) | WO2004087695A1 (de) |
Cited By (5)
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---|---|---|---|---|
WO2006042634A1 (de) * | 2004-10-15 | 2006-04-27 | Saltigo Gmbh | 4-aminophenyl-morpholinon-derivate zur behandlung von hepatitis c |
EP1684744A2 (de) * | 2003-10-01 | 2006-08-02 | Bristol-Myers Squibb Company | Pyrrolidin- und piperidin-derivate als faktor-xa-hemmer |
EP1818330A1 (de) * | 2006-02-14 | 2007-08-15 | Boehringer Ingelheim Pharma GmbH & Co.KG | Substituierte Prolinamide, deren Herstellung und deren Verwendung als Arzneimittel |
WO2007131982A2 (de) | 2006-05-16 | 2007-11-22 | Boehringer Ingelheim International Gmbh | Substituierte prolinamide, deren herstellung und deren verwendung als arzneimittel |
JP2009515925A (ja) * | 2005-11-16 | 2009-04-16 | エフ.ホフマン−ラ ロシュ アーゲー | 凝固第Xa因子のインヒビターとしての新規なピロリジン誘導体 |
Families Citing this family (22)
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DE102004004731A1 (de) * | 2004-01-30 | 2005-08-18 | Merck Patent Gmbh | Harnstoffderivate |
DE102004045796A1 (de) * | 2004-09-22 | 2006-03-23 | Merck Patent Gmbh | Arzneimittel enthaltend Carbonylverbindungen sowie deren Verwendung |
DE102004047254A1 (de) * | 2004-09-29 | 2006-04-13 | Merck Patent Gmbh | Carbonylverbindungen |
US7301817B2 (en) * | 2005-10-27 | 2007-11-27 | Sandisk Corporation | Method for programming of multi-state non-volatile memory using smart verify |
US8673920B2 (en) * | 2009-05-06 | 2014-03-18 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
US9073882B2 (en) | 2010-10-27 | 2015-07-07 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
EP2632464B1 (de) | 2010-10-29 | 2015-04-29 | Merck Sharp & Dohme Corp. | Inhibitoren des renalen kaliumkanals der äusseren medulla |
AU2012299227A1 (en) | 2011-08-19 | 2014-02-20 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
TW201317213A (zh) | 2011-09-16 | 2013-05-01 | Merck Sharp & Dohme | 腎外髓質鉀通道抑制劑 |
WO2013062892A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
WO2013062900A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
WO2013066718A2 (en) | 2011-10-31 | 2013-05-10 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
US9139585B2 (en) | 2011-10-31 | 2015-09-22 | Merck Sharp & Dohme Corp. | Inhibitors of the Renal Outer Medullary Potassium channel |
US9108947B2 (en) | 2011-10-31 | 2015-08-18 | Merck Sharp & Dohme Corp. | Inhibitors of the Renal Outer Medullary Potassium channel |
WO2013090271A1 (en) | 2011-12-16 | 2013-06-20 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
AR092031A1 (es) | 2012-07-26 | 2015-03-18 | Merck Sharp & Dohme | Inhibidores del canal de potasio medular externo renal |
US9777002B2 (en) | 2012-11-29 | 2017-10-03 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
US9573961B2 (en) | 2012-12-19 | 2017-02-21 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
WO2014126944A2 (en) | 2013-02-18 | 2014-08-21 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
EP2968288B1 (de) | 2013-03-15 | 2018-07-04 | Merck Sharp & Dohme Corp. | Inhibitoren des renalen kaliumkanals der äusseren medulla |
WO2015017305A1 (en) | 2013-07-31 | 2015-02-05 | Merck Sharp & Dohme Corp | Inhibitors of the renal outer medullary potassium channel |
WO2015065866A1 (en) | 2013-10-31 | 2015-05-07 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
Citations (2)
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US4217130A (en) * | 1977-10-29 | 1980-08-12 | Kyowa Hakko Kogyo Co., Ltd. | Agents for and method of modifying citrus fruit |
JPS63232846A (ja) * | 1987-03-20 | 1988-09-28 | Haruo Ogura | 新規な固定相担体 |
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WO1998022432A1 (fr) * | 1996-11-18 | 1998-05-28 | Yamanouchi Pharmaceutical Co., Ltd. | Derives d'acylanilide a substitution acylamino ou composition comprenant ces derives |
US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
-
2003
- 2003-07-01 DE DE10329457A patent/DE10329457A1/de not_active Withdrawn
-
2004
- 2004-03-09 WO PCT/EP2004/002405 patent/WO2004087695A1/de active IP Right Grant
- 2004-03-09 PL PL377138A patent/PL377138A1/pl unknown
- 2004-03-09 CA CA2520893A patent/CA2520893C/en not_active Expired - Fee Related
- 2004-03-09 ES ES04718646T patent/ES2287708T3/es not_active Expired - Lifetime
- 2004-03-09 AU AU2004226280A patent/AU2004226280B2/en not_active Ceased
- 2004-03-09 MX MXPA05010433A patent/MXPA05010433A/es not_active Application Discontinuation
- 2004-03-09 KR KR1020057018640A patent/KR20050118709A/ko not_active Application Discontinuation
- 2004-03-09 JP JP2006504602A patent/JP4634369B2/ja not_active Expired - Fee Related
- 2004-03-09 US US10/551,670 patent/US7504500B2/en not_active Expired - Fee Related
- 2004-03-09 AT AT04718646T patent/ATE366732T1/de not_active IP Right Cessation
- 2004-03-09 EP EP04718646A patent/EP1608646B1/de not_active Expired - Lifetime
- 2004-03-09 BR BRPI0408888-3A patent/BRPI0408888A/pt not_active Application Discontinuation
- 2004-03-09 DE DE502004004294T patent/DE502004004294D1/de not_active Expired - Lifetime
- 2004-03-31 TW TW093108904A patent/TW200500339A/zh unknown
- 2004-04-02 PE PE2004000349A patent/PE20050395A1/es not_active Application Discontinuation
- 2004-04-02 AR ARP040101113A patent/AR043831A1/es unknown
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4217130A (en) * | 1977-10-29 | 1980-08-12 | Kyowa Hakko Kogyo Co., Ltd. | Agents for and method of modifying citrus fruit |
JPS63232846A (ja) * | 1987-03-20 | 1988-09-28 | Haruo Ogura | 新規な固定相担体 |
Non-Patent Citations (1)
Title |
---|
DATABASE CAPLUS [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 1989, OGURA, HARUO ET AL: "A process for preparing succinimidyl carbamate or oxamate-containing chromatography carriers and their use for enzyme mobilization and preparation of chromatographic chiral stationary phases", XP002283918, retrieved from STN Database accession no. 1989:595406 * |
Cited By (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1684744A4 (de) * | 2003-10-01 | 2008-12-17 | Bristol Myers Squibb Co | Pyrrolidin- und piperidin-derivate als faktor-xa-hemmer |
EP1684744A2 (de) * | 2003-10-01 | 2006-08-02 | Bristol-Myers Squibb Company | Pyrrolidin- und piperidin-derivate als faktor-xa-hemmer |
WO2006042634A1 (de) * | 2004-10-15 | 2006-04-27 | Saltigo Gmbh | 4-aminophenyl-morpholinon-derivate zur behandlung von hepatitis c |
JP2009515925A (ja) * | 2005-11-16 | 2009-04-16 | エフ.ホフマン−ラ ロシュ アーゲー | 凝固第Xa因子のインヒビターとしての新規なピロリジン誘導体 |
WO2007093595A1 (de) * | 2006-02-14 | 2007-08-23 | Boehringer Ingelheim International Gmbh | Substituierte prolinamide, deren herstellung und deren verwendung als arzneimittel |
EP1818330A1 (de) * | 2006-02-14 | 2007-08-15 | Boehringer Ingelheim Pharma GmbH & Co.KG | Substituierte Prolinamide, deren Herstellung und deren Verwendung als Arzneimittel |
JP2009526813A (ja) * | 2006-02-14 | 2009-07-23 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換プロリンアミド、これらの調製及び医薬組成物としてのこれらの使用 |
US8003639B2 (en) | 2006-02-14 | 2011-08-23 | Boehringer Ingelheim International Gmbh | Substituted prolinamides, the preparation thereof and the use thereof as pharmaceutical compositions |
WO2007131982A3 (de) * | 2006-05-16 | 2008-01-10 | Boehringer Ingelheim Int | Substituierte prolinamide, deren herstellung und deren verwendung als arzneimittel |
WO2007131982A2 (de) | 2006-05-16 | 2007-11-22 | Boehringer Ingelheim International Gmbh | Substituierte prolinamide, deren herstellung und deren verwendung als arzneimittel |
JP2009537483A (ja) * | 2006-05-16 | 2009-10-29 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換プロリンアミド、その製造及び薬物としての使用 |
US7807693B2 (en) | 2006-05-16 | 2010-10-05 | Boehringer Ingelheim International Gmbh | Substituted prolinamides, manufacturing, and the use thereof as medicaments |
KR101422456B1 (ko) | 2006-05-16 | 2014-07-23 | 베링거 인겔하임 인터내셔날 게엠베하 | 치환된 프롤린아미드, 이의 제조방법 및 약물로서의 이의 용도 |
Also Published As
Publication number | Publication date |
---|---|
ES2287708T3 (es) | 2007-12-16 |
KR20050118709A (ko) | 2005-12-19 |
DE502004004294D1 (de) | 2007-08-23 |
AU2004226280B2 (en) | 2010-06-17 |
MXPA05010433A (es) | 2005-11-04 |
CA2520893A1 (en) | 2004-10-14 |
DE10329457A1 (de) | 2005-01-20 |
AR043831A1 (es) | 2005-08-17 |
CA2520893C (en) | 2012-07-10 |
US20060211692A1 (en) | 2006-09-21 |
US7504500B2 (en) | 2009-03-17 |
JP4634369B2 (ja) | 2011-02-16 |
AU2004226280A1 (en) | 2004-10-14 |
EP1608646A1 (de) | 2005-12-28 |
JP2006522037A (ja) | 2006-09-28 |
ATE366732T1 (de) | 2007-08-15 |
PL377138A1 (pl) | 2006-01-23 |
EP1608646B1 (de) | 2007-07-11 |
TW200500339A (en) | 2005-01-01 |
PE20050395A1 (es) | 2005-06-04 |
BRPI0408888A (pt) | 2006-04-11 |
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